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Details

Stereochemistry ACHIRAL
Molecular Formula C45H50ClN7O7S
Molecular Weight 868.439
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VENETOCLAX

SMILES

CC1(C)CCC(CN2CCN(CC2)C3=CC=C(C(=O)NS(=O)(=O)C4=CC=C(NCC5CCOCC5)C(=C4)[N+]([O-])=O)C(OC6=CN=C7NC=CC7=C6)=C3)=C(C1)C8=CC=C(Cl)C=C8

InChI

InChIKey=LQBVNQSMGBZMKD-UHFFFAOYSA-N
InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54)

HIDE SMILES / InChI

Description

Venetoclax (trade name Venclexta, also known as ABT-199) is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an antiapoptotic protein. BCL-2 and its related proteins BCL-XL and MCL-1 bind to and sequester pro-apoptotic signals in the cell, causing a down-regulation of apoptosis. As an oncogene and an important regulator of apoptosis, BCL-2 overexpression therefore results in increased tumor cell survival and resistance to chemotherapy. FDA approved Venetoclax in April 2016 for the treatment of patients with chronic lymphocytic leukemia (CLL) with 17p deletion, as detected by an FDA approved test, who have received at least one prior therapy. Also this drug in phase 3 clinical trial in combination therapy for the treatment patients with refractory myeloma and Acute Myeloid Leukemia. Common side effects include neutropenia, nausea, anemia, diarrhea, upper respiratory tract infection. Major side effects include tumor lysis syndrome and severe neutropenia.

Originator

Approval Year

2016
495
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
VENCLEXTA

Approved Use

VENCLEXTA is a BCL-2 inhibitor indicated for the treatment of patients with chronic lymphocytic leukemia (CLL) with 17p deletion, as detected by an FDA approved test, who have received at least one prior therapy. This indication is approved under accelerated approval based on overall response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.

Launch Date

1.46033279E12
Primary
Phase III
656
Unknown

Approved Use

Unknown
Primary
Phase III
656
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.1 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: LOW-FAT
1.43 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27558232
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
32.8 μg × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: LOW-FAT
30.2 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27558232
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
14.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27558232
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: LOW-FAT
Doses

Doses

DosePopulationAdverse events​
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Disc. AE: Nausea, Diarrhea...
Other AEs: Nausea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Nausea (5 patients)
Diarrhea (4 patients)
Other AEs:
Nausea (grade 1-2, 53%)
Diarrhea (grade 1-2, 53%)
Diarrhea (grade 3-4, 2%)
Fatigue (grade 1-2, 49%)
Fatigue (grade 3-4, 6%)
Decreased appetite (grade 1-2, 29%)
Vomiting (grade 1-2, 24%)
Constipation (grade 1-2, 18%)
Headache (grade 1-2, 20%)
Anemia (grade 1-2, 10%)
Anemia (grade 3-4, 8%)
Cough (grade 1-2, 10%)
Neutropenia (grade 1-2, 12%)
Neutropenia (grade 3-4, 8%)
Back pain (grade 1-2, 16%)
Back pain (grade 3-4, 2%)
Upper respiratory tract infection (grade 1-2, 8%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Disc. AE: Neutropenia, Thrombocytopenia...
Other AEs: Neutropenia, Neutrophil count decreased...
AEs leading to
discontinuation/dose reduction:
Neutropenia (grade 3-4, 41%)
Thrombocytopenia (grade 3-4, 15%)
Febrile neutropenia (serious, 2%)
Anemia hemolytic autoimmune (serious, 2%)
Other AEs:
Neutropenia (all grades, > 20)
Neutrophil count decreased (all grades, 45%)
Neutrophil count decreased (grade 3-4, 41%)
Diarrhea (all grades, > 20)
Diarrhea (grade 3-4, <1%)
Nausea (grade 3-4, <1%)
Nausea (all grades, > 20)
Anemia (all grades, > 20)
Anemia (grade 3-4, 18%)
Hemoglobin decreased (all grades, 29%)
Hemoglobin decreased (grade 3-4, 18%)
Upper respiratory tract infection (all grades, > 20)
Thrombocytopenia (all grades, > 20)
Platelet count decreased (all grades, 22%)
Platelet count decreased (grade 3-4, 15%)
Fatigue (all grades, > 20)
Fatigue (grade 3-4, 2%)
Pneumonia (serious, 2%)
Pyrexia (serious, 2%)
Anemia (serious, 2%)
Tumor lysis syndrome (serious, 2%)
Vomiting (all grades, 15%)
Vomiting (grade 3-4, <1%)
Constipation (all grades, 14%)
Peripheral edema (all grades, 11%)
Peripheral edema (grade 3-4, <1%)
Upper respiratory tract infection (all grades, 22%)
Upper respiratory tract infection (grade 3-4, 1%)
Pneumonia (all grades, 8%)
Pneumonia (grade 3-4, 5%)
Hypokalemia (all grades, 12%)
Hypokalemia (grade 3-4, 4%)
Back pain (all grades, 10%)
Back pain (grade 3-4, <1%)
Headache (all grades, 15%)
Headache (grade 3-4, <1%)
Cough (all grades, 13%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
unhealthy
n = 9
Health Status: unhealthy
Condition: relapsed/refractory MM
Population Size: 9
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
DLT: Nausea, Abdominal pain...
Dose limiting toxicities:
Nausea (grade 3, 1 patient)
Abdominal pain (grade 2, 1 patient)
Vomiting (grade 3, 1 patient)
Epigastralgia (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
AEs

AEs

AESignificanceDosePopulation
Diarrhea 4 patients
Disc. AE
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Nausea 5 patients
Disc. AE
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Anemia grade 1-2, 10%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Cough grade 1-2, 10%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Neutropenia grade 1-2, 12%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Back pain grade 1-2, 16%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Constipation grade 1-2, 18%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Headache grade 1-2, 20%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Vomiting grade 1-2, 24%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Decreased appetite grade 1-2, 29%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Fatigue grade 1-2, 49%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Diarrhea grade 1-2, 53%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Nausea grade 1-2, 53%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Upper respiratory tract infection grade 1-2, 8%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Back pain grade 3-4, 2%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Diarrhea grade 3-4, 2%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Fatigue grade 3-4, 6%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Anemia grade 3-4, 8%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Neutropenia grade 3-4, 8%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
unhealthy, 66 years (range: 25 - 86 years)
n = 52
Health Status: unhealthy
Condition: Relapsed or Refractory Non-Hodgkin Lymphoma
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Population Size: 52
Sources:
https://pubmed.ncbi.nlm.nih.gov/28095146
Back pain all grades, 10%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Peripheral edema all grades, 11%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Hypokalemia all grades, 12%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Cough all grades, 13%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Constipation all grades, 14%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Headache all grades, 15%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Vomiting all grades, 15%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Platelet count decreased all grades, 22%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Upper respiratory tract infection all grades, 22%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Hemoglobin decreased all grades, 29%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Neutrophil count decreased all grades, 45%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Pneumonia all grades, 8%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Anemia all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Diarrhea all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Fatigue all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Nausea all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Neutropenia all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Thrombocytopenia all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Upper respiratory tract infection all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Upper respiratory tract infection grade 3-4, 1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Platelet count decreased grade 3-4, 15%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Thrombocytopenia grade 3-4, 15%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Anemia grade 3-4, 18%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Hemoglobin decreased grade 3-4, 18%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Fatigue grade 3-4, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Hypokalemia grade 3-4, 4%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Neutrophil count decreased grade 3-4, 41%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Neutropenia grade 3-4, 41%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Pneumonia grade 3-4, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Back pain grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Diarrhea grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Headache grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Nausea grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Peripheral edema grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Vomiting grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Anemia serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Pneumonia serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Pyrexia serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Tumor lysis syndrome serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Anemia hemolytic autoimmune serious, 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Febrile neutropenia serious, 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
unhealthy, 66 years (range: 29 - 85 years)
n = 240
Health Status: unhealthy
Condition: CLL
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Population Size: 240
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf
Abdominal pain grade 2, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
unhealthy
n = 9
Health Status: unhealthy
Condition: relapsed/refractory MM
Population Size: 9
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
Epigastralgia grade 3, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
unhealthy
n = 9
Health Status: unhealthy
Condition: relapsed/refractory MM
Population Size: 9
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
Nausea grade 3, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
unhealthy
n = 9
Health Status: unhealthy
Condition: relapsed/refractory MM
Population Size: 9
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
Vomiting grade 3, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
unhealthy
n = 9
Health Status: unhealthy
Condition: relapsed/refractory MM
Population Size: 9
Sources:
https://pubmed.ncbi.nlm.nih.gov/29018077
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587

inducer
781
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1461

CYP2C8
911

CYP1A2
1524

CYP2B6
810

CYP2C19
1478

BCRP
699
CYP3A4/5
85

P-gp
1537

BCRP
561

OATP1B1
406

OATP1B3
350
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2D6
1891
 no
CYP3A4
1925
 no
CYP3A4
1925
 no
BCRP
773
 yes [IC50 0.13 uM]
CYP2C9
1819
 yes [IC50 0.14 uM]
P-gp
1650
 yes [IC50 0.79 uM]
CYP2C8
965
 yes [IC50 0.82 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4/5
85
 major
yes (co-administration study)
Comment: Co-administration of ketoconazole (a strong CYP3A, P-gp and BCRP inhibitor) increased venetoclax Cmax and AUCX by 2.3- and 6.4-fold, respectively. Co-administration of moderate CYP3A4/5 inhibitors showed a smaller effect on venetoclax exposrue (40 to 60% increase in Cmax and AUCo-24)-
Page: 6.0
OATP1B1
406
 no
OATP1B3
350
 no
BCRP
561
 yes
P-gp
1537
 yes
yes (co-administration study)
Comment: Venetoclax exposure also increased (Cmax t 106%, AUCX T 78%) after co-administration of single dose of rifampin, presumably due to the inhibition of P-gp by rifampin.
Page: 6.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:133021
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:133021
ChemicalBook
CB62645962
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62645962
MolPort
MolPort-028-720-431
https://www.molport.com/shop/molecule-link/MolPort-028-720-431
Selleck Chemicals
abt-199
http://www.selleckchem.com/products/abt-199.html
ZINC
ZINC000150338755
http://zinc15.docking.org/substances/ZINC000150338755
PubMed

PubMed

TitleDatePubMed
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
2008 Nov 13
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
2013 Feb
Patents

Patents

20100305122
2
20110124628
2
20120028925
2
JP2013543894A
2

Sample Use Guides

In Vivo Use Guide
Initiate therapy with VENCLEXTA (venetoclax) at 20 mg once daily for 7 days, followed by a weekly ramp-up dosing schedule to the recommended daily dose of 400 mg. VENCLEXTA tablets should be taken orally once daily with a meal and water.
Route of Administration: Oral
In Vitro Use Guide
ABT-199 (Venetoclax) shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM.
Name Type Language
VENETOCLAX
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
RG7601
Code English
ABT-199
Code English
venetoclax [INN]
Common Name English
VENCLEXTA
Brand Name English
VENETOCLAX [ORANGE BOOK]
Common Name English
Venetoclax [WHO-DD]
Common Name English
VENETOCLAX [USAN]
Common Name English
4-(4-((2-(4-CHLOROPHENYL)-4,4-DIMETHYLCYCLOHEX-1-EN-1-YL)METHYL)PIPERAZIN-1-YL)-N-((3-NITRO-4-((TETRAHYDRO-2HPYRAN-4-YLMETHYL) AMINO)PHENYL)SULFONYL)-2-(1H-PYRROLO(2,3-B)PYRIDIN-5-YLOXY)BENZAMIDE
Common Name English
RG-7601
Code English
VENETOCLAX [MI]
Common Name English
BENZAMIDE, 4-(4-((2-(4-CHLOROPHENYL)-4,4-DIMETHYL-1-CYCLOHEXEN-1-YL)METHYL)-1-PIPERAZINYL)-N-((3-NITRO-4-(((TETRAHYDRO-2H-PYRAN-4-YL)METHYL)AMINO)PHENYL)SULFONYL)-2-(1H-PYRROLO(2,3-B)PYRIDIN-5-YLOXY)-
Common Name English
VENETOCLAX [JAN]
Common Name English
4-(4-((2-(4-CHLOROPHENYL)-4,4-DIMETHYLCYCLOHEX-1-EN-1-YL)METHYL)PIPERAZIN-1-YL)-N-((3-NITRO-4-((TETRAHYDRO-2H-PYRAN-4-YLMETHYL)AMINO)PHENYL)SULFONYL)-2-(1H-PYRROLO(2,3-B)PYRIDIN-5-YLOXY)BENZAMIDE
Systematic Name English
GDC-0199
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 375612
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
NDF-RT N0000192515
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 536116
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
EU-Orphan Drug EU/3/16/1617
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 780920
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 664118
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 423814
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 777520
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
NCI_THESAURUS C129824
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
WHO-ATC L01XX52
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 689119
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 600117
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
FDA ORPHAN DRUG 506815
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
Code System Code Type Description
RXCUI
1747556
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
NCI_THESAURUS
C103147
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
EVMPD
SUB176260
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
PUBCHEM
49846579
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
USAN
AB-76
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
WIKIPEDIA
Venetoclax
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
SMS_ID
100000162440
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
DRUG CENTRAL
5133
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
EPA CompTox
DTXSID30154863
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
FDA UNII
N54AIC43PW
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
CAS
1257044-40-8
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
NDF-RT
N0000009176
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY Increased Cellular Death [PE]
DAILYMED
N54AIC43PW
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
NDF-RT
N0000185503
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY P-Glycoprotein Inhibitors [MoA]
ChEMBL
CHEMBL3137309
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
INN
9925
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
DRUG BANK
DB11581
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
MERCK INDEX
m11932
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
CHEBI
133021
Created by admin on Sat Dec 16 05:11:35 UTC 2023 , Edited by admin on Sat Dec 16 05:11:35 UTC 2023
PRIMARY
ACTIVE MOIETY
Structure of VENETOCLAX
NIH
NCATS
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ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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